Hycanthone is the

schistosomicide A schistosomicide is a drug used to combat schistosomiasis. List Examples listed in MeSH include: * amoscanate * arteether * artemether * chloroxylenol * hycanthone * lucanthone * metrifonate * niridazole * oltipraz * oxamniquine * praziquante ...

approved by the FDA in 1975. It is a metabolite of lucanthone. Hycanthone interferes with

parasite Parasitism is a Symbiosis, close relationship between species, where one organism, the parasite, lives (at least some of the time) on or inside another organism, the Host (biology), host, causing it some harm, and is Adaptation, adapted str ...

nerve function, resulting in

paralysis Paralysis (: paralyses; also known as plegia) is a loss of Motor skill, motor function in one or more Skeletal muscle, muscles. Paralysis can also be accompanied by a loss of feeling (sensory loss) in the affected area if there is sensory d ...

and death. This agent also intercalates into DNA and inhibits RNA synthesis ''

in vitro ''In vitro'' (meaning ''in glass'', or ''in the glass'') Research, studies are performed with Cell (biology), cells or biological molecules outside their normal biological context. Colloquially called "test-tube experiments", these studies in ...

'' and shows potential antineoplastic activity.

Anti-schistosomal activity

Hycanthone is shown to be an effective inhibitor of

acetylcholinesterase Acetylcholinesterase (HUGO Gene Nomenclature Committee, HGNC symbol ACHE; EC 3.1.1.7; systematic name acetylcholine acetylhydrolase), also known as AChE, AChase or acetylhydrolase, is the primary cholinesterase in the body. It is an enzyme th ...

(AChE) from ''

Schistosoma mansoni A paired couple of ''Schistosoma mansoni''. ''Schistosoma mansoni'' is a water-borne parasite of humans, and belongs to the group of blood flukes (''Schistosoma''). The adult lives in the blood vessels ( mesenteric veins) near the human inte ...

'', but is less potential against AChE from mammalian origin. This might come from differences in the configuration of active center between schistosome and mammalian AChE enzymes. Hycanthone is shown to

intercalate Intercalation may refer to: *Intercalation (chemistry), insertion of a molecule (or ion) into layered solids such as graphite *Intercalation (timekeeping), insertion of a leap day, week or month into some calendar years to make the calendar follo ...

into DNA and inhibit RNA synthesis ''

''. A growing body of evidence has shown that hycathone has an antineoplastic activity.

Toxicity

Hycanthone is a dose-dependent

hepatotoxin A hepatotoxin (''Greek language, Gr., hepato = liver'') is a toxic chemical substance that damages the liver. It can be a adverse effect, side-effect, but hepatotoxins are also found naturally, such as microcystins and pyrrolizidine alkaloids, or ...

, causing hepatocellular injury.

Clinical trials

* Phase II Study of Chemotherapy with Hycanthone for Advanced Colorectal Carcinoma. * Phase II Chemotherapy with Hycanthone Mesylate and Flagyl for Advanced Malignant Lymphomas (Completed)

Physical properties

References

{{Anthelmintics Antiparasitic agents Thioxanthones Diethylamino compounds